Description
KB02-SLF is a PROTAC-based nuclear FKBP12 degrader (molecular glue). KB02-SLF promotes nuclear FKBP12 degradation by covalently modifying DCAF16 (E3 ligase) and can improve the durability of protein degradation in biological systems. SLF binds ubiquitin E3 ligase ligand KB02 via a linker to form KB02-SLFIn VitroKB02-SLF (2 µM; 4-72 hours; HEK293T cells) treatment promotes a substantial reduction in nuclear FKBP12 that is sustained across a 4-72 h time frame. Cell imaging studies confirms the selective loss of nuclear-localized FKBP12 in KB02-SLF-treated cells. KB02-SLF promotes the loss of FKBP12_NLS across a concentration of ~0.5-5µM, but shows varied reductions in activity at higher concentrations. The degradation of FKBP12_NLS induced by KB02-SLF is mediated by DCAF16. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: HEK293T cells Concentration: 2 µM Incubation Time: 4 hours, 8 hours, 24 hours, 48 hours, 72 hours Result: Promoted a substantial reduction in nuclear FKBP12 that was sustained across a 4-72 h time frame.Form:SolidIC50& Target:FKBP12